Experimental and Clinical Investigation of a Non-Hormonal Anti-Inflammatory Eye Ointment

Abstract

The penetration of [¹⁴C]-labelled oxyphenbutazone (OPB = active substance of Tanderil® eye ointment) from a 10-percent eye ointment into the various tissues was investigated in the rabbit eye and the human eye. A decline in the OPB concentration progressing from the cornea to the posterior sections of the eye was observed in both rabbit and human. The percentage distribution of [¹⁴C]-OPB in the human eye revealed that the highest values were recorded for the cornea and sclera and the lowest values for the lens and vitreous body. The capsule of bovine lenses permits the penetration of OPB, which is then found in a higher concentration in the periphery than in the nucleus of the lens. OPB in 10^––4 m concentration in the nutrient medium for calf and bovine lenses did not influence carbohydrate metabolic processes. Only with 10^––2 M OPB in the medium were changes in the metabolism rate produced, e. g. the content of energy-rich phosphates was reduced. After application of a 5- or 10-percent OPB eye ointment no visible lens changes were observed in rats and rabbits. As regards galactose-induced cataracts in young rats and naphthaline-induced cataracts in rabbits, OPB eye ointment (5 and 10%) neither reduced the latent period nor increased the degree of opacity. An additive cataractogenic effect on the part of OPB could therefore be excluded. A 10-percent OPB eye ointment has no influence on the intraocular pressure of either the normal or the glaucomatous human eye, unlike a 2.5-percent prednisolone eye ointment, which increases the pressure in about half of the glaucoma patients. This difference between prednisolone eye ointment and OPB eye ointment as regards the rise in pressure, observed in a double-blind trial, is statistically significant.